PROfind: 68Ga-PSMA-R2 in Patients With Biochemical Relapse (BR) and Metastatic Prostate Cancer (mPCa)

• Sponsor: Advanced Accelerator Applications (Industry)
• Overall Status: Completed
• CT.gov ID: NCT03490032
• Collaborator: (none)
• Enrollment: 30
• Locations: 5
• Arms: 3
• Actual Duration (Months): 15.7
• Patients Per Site: 6
• Patients Per Site Per Month: 0.4

Study Details

Study Description

Brief Summary

This was an open-label, multicenter, single dose, Phase I/II study to evaluate the safety and tolerability of a single administration of 3 mega Becquerel (MBq)/kg, but not less than 150 MBq and not more than 250 MBq, of 68^Ga-PSMA-R2 in adult male patients with biochemical relapse (BR) and metastatic prostate cancer (mPCa).

Condition or Disease	Intervention/Treatment	Phase
Prostate Cancer Metastatic	Drug: [68Ga]-PSMA-R2	Phase 1/Phase 2

Detailed Description

This study consisted of 2 parts.

• During the first part (Phase I) of the study, 6 subjects with biochemically recurrent prostate cancer (PCa) received the investigational product (IP) and remained at the site for approximately 6 hours post-administration in order to assess the PK, biodistribution versus time, and dosimetry for critical organs. Subjects received a single dose of 3 MBq/kg, (>=150 and =<250 MBq), of 68^Ga-PSMA-R2 intravenously. Serial blood and urine samples were collected for PK characterization and dosimetry and whole-body PET/CT were acquired at selected time points (0 to 4 hours) to determine organ and tumor absorbed doses. Safety assessments were conducted after IP administration on Day 1, and during follow-up on Days 7 and 28.

• In the second part of the study (Phase II), 2 groups of 12 subjects were enrolled (subjects with PCa in biochemical recurrence [PCa-BR], and subjects with prostate cancer in the metastatic stage [mPCa]). Based on the preliminary data analysis from the Phase I part of the study provided sufficient dosimetry data, all subjects underwent the whole body PET/CT imaging optimized for time (up to 2 time points) according to the data analysis from the Phase I part of the study.

This study was comprised of 4 clinical visits and conducted in 3 study periods: screening, administration/imaging, and safety follow-up period.

Study Design

• Study Type: Interventional
• Actual Enrollment: 30 participants
• Allocation: Non-Randomized
• Intervention Model: Sequential Assignment
• Intervention Model Description: Phase I: characterize PK and dosimetry Phase II: diagnostic potential in 2 groups Prostate Cancer in biochemical relapse, and Metastatic Prostate CancerPhase I: characterize PK and dosimetry Phase II: diagnostic potential in 2 groups Prostate Cancer in biochemical relapse, and Metastatic Prostate Cancer
• Masking: None (Open Label)
• Primary Purpose: Diagnostic
• Official Title: A Phase 1/2 Open-label, Multi-center, Safety and Tolerability Study of a Single Dose of 68Ga-PSMA-R2 in Patients With Biochemical Relapse (BR) and Metastatic Prostate Cancer (mPCa)
• Actual Study Start Date: May 23, 2018
• Actual Primary Completion Date: Aug 20, 2019
• Actual Study Completion Date: Sep 13, 2019

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I) All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	Drug: [68Ga]-PSMA-R2; radio-labelled PSMA ligand
Experimental: Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II) All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	Drug: [68Ga]-PSMA-R2; radio-labelled PSMA ligand
Experimental: Metastatic Prostate Cancer (mPCa) (Phase II) All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	Drug: [68Ga]-PSMA-R2; radio-labelled PSMA ligand

Outcome Measures

Primary Outcome Measures

1. Number of Participants With Treatment Emergent Adverse Events [dosing through 28 days post-dose]

   Treatment-emergent adverse events (TEAEs) were collected from first dosing (single administration, Day 1) up to last follow-up visit or until the event has resolved to baseline grade or better or the event was assessed stable by the investigator or the patient was lost to follow-up or withdrew consent. The distribution of adverse events was done via the analysis of frequencies for treatment emergent Adverse Event (TEAEs), Serious Adverse Event (TESAEs) and Deaths due to AEs, through the monitoring of relevant clinical and laboratory safety parameters. Only descriptive analysis performed.

Secondary Outcome Measures

1. Phase I: Decay Corrected Tissue Time-activity Curves (TACs) From 68Ga-PSMA-R2 PET/CT Images in Normal Organs [68Ga-PSMA-R2 PET imaging acquired at Day 1 (20-30 min post-injection, 1 hour, 2 hours and 3-4 hours post-injection)]

   PET/CT scans were performed at approximately 20 to 30 min and at 1, 2, 3 to 4 hours postinjection. Time activity curves (TACs) for various organs (Brain, Heart Wall, Kidney, Lacrimal Gland, Liver, Lungs, Salivary Gland, Spleen and Thyroid) were produced as decay-corrected tissue of injected activity (mSv/MBq) per organ. Only descriptive analysis performed.

2. Phase I: Urinary Excretion of [68Ga]-PSMA-R2 [0 to 6 hours post-dose]

   Urine samples were collected (up to 6 hours after dosing) for activity-based pharmacokinetics characterization. The apparent systemic clearance for the analyte in urine (Cl) was summarized with descriptive statistics.

3. Phase I: Half-life of 68Ga-PSMA-R2 in Blood [0 to 6 hours post-dose]

   Serial blood samples were collected (up to 6 hours after dosing) for activity-based pharmacokinetics characterization. The half-life (T^1/2) for the analyte in blood was summarized with descriptive statistics.

4. Phase I: Non-decay Corrected Tissue Time-activity Curves (TACs) From 68Ga-PSMA-R2 PET/CT Images in Normal Organs [68Ga-PSMA-R2 PET imaging acquired at Day 1 (20-30 min post-injection, 1 hour, 2 hours and 3-4 hours post-injection)]

   PET/CT scans were performed at approximately 20 to 30 min and at 1, 2, 3 to 4 hours postinjection. Time activity curves (TACs) for the various organs were produced as non-decay-corrected fraction of injected activity (mSv/MBq) per organ. Only descriptive analysis performed.

5. Phase I: Residence Times in Normal Organs [68Ga-PSMA-R2 PET imaging acquired at Day 1]

   Residence times of radiation in normal organs were summarized with descriptive statistics.

6. Phase I: Absorbed Dose of 68Ga-PSMA-R2 [68Ga-PSMA-R2 PET imaging acquired at Day 1]

   Absorbed radiation dose of 68Ga-PSMA-R2 in target organs were summarized with descriptive statistics.

7. Phase I: Whole-body Dose of 68Ga-PSMA-R2 [68Ga-PSMA-R2 PET imaging acquired at Day 1]

   The whole-body dose of 68Ga-PSMA-R2 was summarized with descriptive statistics.

8. Phase I: Effective Dose of 68Ga-PSMA-R2 [68Ga-PSMA-R2 PET imaging acquired at Day 1]

   The effective dose of 68Ga-PSMA-R2 was summarized with descriptive statistics.

9. Standard Uptake Value (SUV) Mean and Max in Lesions Detected by PET Scans by Timepoint [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

   Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The SUVmean and SUVmax (g/mL) of each lesion were calculated and reported by lesion location with summary statistics at all imaging time points.

10. Tumor to Background Ratio (TBR) of Lesions Detected by PET Scans by Timepoint [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

    Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The lesion Tumor to Background Ratio (TBR) was defined as SUVmax(lesion) / SUVmean(gluteal or thigh) was calculated and reported by lesion location with summary statistics at all imaging time points.

11. Standard Uptake Value (SUV) Mean and Max in Lesions Detected by PET Scans and Also Detected by Conventional Scans by Timepoint [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

    Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The SUVmean and SUVmax (g/mL) of each lesion were calculated and reported by lesion location with summary statistics at all imaging time points.

12. Tumor to Background Ratio (TBR) of Lesions Detected by PET Scans and Also Detected by Conventional Scans by Timepoint [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

    Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The lesion Tumor to Background Ratio (TBR) was defined as SUVmax(lesion) / SUVmean(gluteal or thigh) was calculated and reported by lesion location with summary statistics at all imaging time points.

13. Standard Uptake Value (SUV) Mean and Max in Lesions Detected by PET Scans and Not Detected by Conventional Scans by Timepoint [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

    Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The SUVmean and SUVmax (g/mL) of each lesion were calculated and reported by lesion location with summary statistics at all imaging time points.

14. Tumor to Background Ratio (TBR) of Lesions Detected by PET Scans and Not Detected by Conventional Scans by Timepoint [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

    Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The lesion Tumor to Background Ratio (TBR) was defined as SUVmax(lesion) / SUVmean(gluteal or thigh) was calculated and reported by lesion location with summary statistics at all imaging time points.

15. Patient Level Agreement of 68Ga-PSMA-R2 PET Imaging Relative to Conventional Techniques in Prostate Cancer Patients [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)]

    The subject-level positive percent agreement, negative percent agreement, and overall percent agreement was calculated based on the number of subjects with at least 1 positive lesion detected by conventional scan or at least 1 positive lesion detected by PET scan. These percent agreements were calculated as follows: Positive percent agreement: a/(a+c) × 100 Negative percent agreement: d/(b+d) × 100 Overall percent agreement: (a+d)/(a+b+c+d) × 100 Where: a = number of subjects with at least 1 positive lesion detected by conventional scan and at least 1 positive lesion detected by PET scan b = number of subjects with at least 1 positive lesion detected by PET scan that was not correlated with conventional scan c = number of subjects with at least 1 positive lesion detected by conventional scan that was not correlated with PET scan d = number of subjects with no lesions detected by conventional scan or PET scan.

16. Burden of Tumor Lesions Measured by 68Ga-PSMA-R2 PET (1hr) Scan Compared With Standard Imaging Modality, by Location (Overall) [68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour post-injection)]

    The differences of number of positive lesions, number of positive lesions detected by PET scan and/or conventional scan and the location of positive lesions were summarized with descriptive statistics.

Eligibility Criteria

Criteria

• Ages Eligible for Study: 18 Years and Older
• Sexes Eligible for Study: Male
• Accepts Healthy Volunteers: No

Inclusion Criteria:

1. Males 18 years or older.

2. Signed and dated written informed consent by the subject prior to any study-specific procedures.

3. Histologically confirmed adenocarcinoma of the prostate, defined as follows:

4. Biochemical recurrence: defined as PSA is ≥0.2 ng/mL after radical prostatectomy or PSA nadir plus 2 ng/mL after radiation therapy with corresponding CT/MRI or bone scan revealing absence of local recurrence or metastatic lesions.

OR

1. Metastatic disease: defined as both, castration-sensitive or castration-resistant mPCa (presence of at least 1 metastatic lymph node, visceral metastasis and/or bone metastasis).

2. At least 2 weeks must have elapsed between last anticancer treatment administration and the administration of the imaging product, 68Ga-PSMA-R2.

3. Prior major surgery must be at least 12 weeks prior to study entry.

4. Eastern Cooperative Oncology Group (ECOG) performance status 0 to 2, with a life expectancy ≥6 months.

5. Adequate bone marrow reserve and organ function as demonstrated by complete blood count, and biochemistry in blood and urine at Screening:

6. Hemoglobin (Hb): >8 g/dL

7. Platelet count of >50.000/mm3

8. Serum creatinine <1.5*upper limit normal (ULN) or estimated glomerular filtration rate (eGFR) >50 mL/min based upon The Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) equation.

9. For male subjects with partners of childbearing potential, agreement to use barrier contraceptive method (condom) and to continue its use for 28 days after IP administration.

Exclusion Criteria:

1. Pathological finding consistent with small cell, neuroendocrine carcinoma of the prostate or any other histologies different than adenocarcinoma.

2. Administered a radioisotope =<10 physical half-lives prior to the day of PET/CT.

3. Current severe urinary incontinence, hydronephrosis, severe voiding dysfunction, or need of indwelling/condom catheters.

4. Uncontrolled pain or incompatibility that results in subject's lack of compliance with imaging procedures.

5. Other known coexisting malignancies except non-melanoma skin or low grade superficial bladder cancer unless definitively treated and proven no evidence of recurrence for 5 years.

6. Subject with known incompatibility to CT scans.

7. Any evidence of severe or uncontrolled systemic or psychiatric diseases, including uncontrolled hypertension and active bleeding diatheses, which in the investigator's opinion makes it undesirable for the subject to participate in the study or which would jeopardize compliance with the protocol, or active infection including human immunodeficiency virus (HIV) and untreated hepatitis B, hepatitis C. Screening for chronic conditions was not required.

8. Subjects who have received any investigational agent within the last 28 days were excluded from participation in this study.

9. Any acute toxicity due to prior chemotherapy and/or radiotherapy that has not resolved according to the Toxicity Grading Scale for Healthy Adult and Adolescent Volunteers Enrolled in Preventive Vaccine Clinical Studies.

10. Known allergy, hypersensitivity, or intolerance to the IP or its excipients.

11. Subject unlikely to comply with study procedures, restrictions and requirements and judged by the investigator to be unsuitable for study participation.

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	Pheonix Molecular Imaging Center	Phoenix	Arizona	United States	85040
2	University of California, San Francisco (UCSF)	San Francisco	California	United States	94158
3	Smilow Cancer Center at Yale New Haven	New Haven	Connecticut	United States	06510
4	Johns Hopkins Hospital	Baltimore	Maryland	United States	21287
5	National Institutes of Health, Warren Grant Magnusen Clinical Center	Bethesda	Maryland	United States	20892

Sponsors and Collaborators

• Advanced Accelerator Applications

Investigators

• Study Director: Novartis Pharmaceuticals, Novartis Pharmaceuticals

Study Documents (Full-Text)

• Statistical Analysis Plan - Jun 29, 2020
• Study Protocol - Feb 22, 2018

More Information

Publications

None provided.

• Responsible Party: Advanced Accelerator Applications
• ClinicalTrials.gov Identifier: NCT03490032
• Other Study ID Numbers: A206D-A01-001; CAAA502A12101
• First Posted: Apr 6, 2018
• Last Update Posted: Nov 17, 2020
• Last Verified: Oct 1, 2020

• Individual Participant Data (IPD) Sharing Statement: Yes
• Plan to Share IPD: Yes
• Studies a U.S. FDA-regulated Drug Product: Yes
• Studies a U.S. FDA-regulated Device Product: No
• Keywords provided by Advanced Accelerator Applications: Prostatic Neoplasms; Cancer of Prostate; Cancer of the Prostate; Neoplasms, Prostate; Prostate Cancer; Prostatic Cancer; Genital Neoplasms, Male; Urogenital Neoplasms; Neoplasms by Site; Neoplasms; Genital Diseases, Male; Prostatic Diseases; PSMA; Prostate-specific membrane antigen; Gallium radioisotope 68; 68Ga-PSMA-R2; 68Ga-PSMA ligand
• Additional relevant MeSH terms: Prostatic Neoplasms

Study Results

Participant Flow

Recruitment Details	This study was conducted at 5 centers in the USA (Phase I: 1 site; Phase II: 4 sites)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Period Title: Overall Study
STARTED	6	12	12
COMPLETED	5	12	12
NOT COMPLETED	1	0	0

Baseline Characteristics

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)	Total
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	Total of all reporting groups
Overall Participants	6	12	12	30
Age (Years) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Years]	66.2 (7.91)	69.1 (6.53)	68.6 (10.00)	68.3 (8.13)
Sex: Female, Male (Count of Participants)
Female	0 0%	0 0%	0 0%	0 0%
Male	6 100%	12 100%	12 100%	30 100%
Race/Ethnicity, Customized (Number) [Number]
Asian	0 0%	1 8.3%	0 0%	1 3.3%
White	6 100%	10 83.3%	11 91.7%	27 90%
Other	0 0%	1 8.3%	1 8.3%	2 6.7%
ECOG Performance Status (Count of Participants)
Grade 0	6 100%	9 75%	6 50%	21 70%
> = Grade 1	0 0%	3 25%	6 50%	9 30%
Prostate-specific antigen (PSA) levels (ng/mL) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [ng/mL]	1.68 (1.329)	3.72 (6.461)	38.56 (66.603)	17.25 (44.861)
Time since first prostate cancer diagnosis (Months) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Months]	79.2 (46.44)	86.8 (78.07)	96.1 (84.80)	88.8 (73.41)
Time since first metastasis (Months) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Months]	79.2 (46.44)	86.8 (78.07)	96.1 (84.80)	88.8 (73.41)
Time since disease progression (Months) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Months]	34.7 (33.02)	1.2 (1.55)	0.8 (0.65)	5.8 (16.01)
Number of patients by castration type (Count of Participants)
Surgery	0 0%	10 83.3%	4 33.3%	14 46.7%
Pharmacological	1 16.7%	3 25%	11 91.7%	15 50%
Not Applicable	1 16.7%	1 8.3%	0 0%	2 6.7%
Number of patients by Primary and Secondary Gleason score (Count of Participants)
Primary Gleason score=3 &Secondary Gleason score=3	0 0%	2 16.7%	2 16.7%	4 13.3%
Primary Gleason score=3 &Secondary Gleason score=4	2 33.3%	4 33.3%	0 0%	6 20%
Primary Gleason score=4 &Secondary Gleason score=3	2 33.3%	4 33.3%	3 25%	9 30%
Primary Gleason score=4 &Secondary Gleason score=4	0 0%	1 8.3%	3 25%	4 13.3%
Primary Gleason score=4 &Secondary Gleason score=5	2 33.3%	1 8.3%	4 33.3%	7 23.3%
Number of patients by Total Gleason score (>=6) (Count of Participants)
6	0 0%	2 16.7%	2 16.7%	4 13.3%
7	4 66.7%	8 66.7%	3 25%	15 50%
8	0 0%	1 8.3%	3 25%	4 13.3%
9	2 33.3%	1 8.3%	4 33.3%	7 23.3%
10	0 0%	0 0%	0 0%	0 0%
Baseline Weight (kilogram (kg)) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [kilogram (kg)]	91.48 (18.091)	87.03 (18.838)	93.20 (11.402)	90.29 (15.890)
Baseline Height (centimeter (cm)) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [centimeter (cm)]	183.00 (5.030)	177.96 (6.596)	177.03 (5.927)	178.65 (6.281)

Outcome Measures

1. Primary Outcome

Title	Number of Participants With Treatment Emergent Adverse Events
Description	Treatment-emergent adverse events (TEAEs) were collected from first dosing (single administration, Day 1) up to last follow-up visit or until the event has resolved to baseline grade or better or the event was assessed stable by the investigator or the patient was lost to follow-up or withdrew consent. The distribution of adverse events was done via the analysis of frequencies for treatment emergent Adverse Event (TEAEs), Serious Adverse Event (TESAEs) and Deaths due to AEs, through the monitoring of relevant clinical and laboratory safety parameters. Only descriptive analysis performed.
Time Frame	dosing through 28 days post-dose

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
Treatment-Emergent Adverse Events (TEAEs)	1 16.7%	4 33.3%	2 16.7%
Serious TEAEs	0 0%	1 8.3%	0 0%
Deaths Due to AEs	0 0%	0 0%	0 0%

2. Secondary Outcome

Title	Phase I: Decay Corrected Tissue Time-activity Curves (TACs) From 68Ga-PSMA-R2 PET/CT Images in Normal Organs
Description	PET/CT scans were performed at approximately 20 to 30 min and at 1, 2, 3 to 4 hours postinjection. Time activity curves (TACs) for various organs (Brain, Heart Wall, Kidney, Lacrimal Gland, Liver, Lungs, Salivary Gland, Spleen and Thyroid) were produced as decay-corrected tissue of injected activity (mSv/MBq) per organ. Only descriptive analysis performed.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (20-30 min post-injection, 1 hour, 2 hours and 3-4 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS). Only participants with a value at each post-injection timepoints were included in the analysis.

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Brain@20-30 minutes post-injection	0.002196 (0.0009359)
Brain@1 hour post-injection	0.001913 (0.0003011)
Brain@2 hours post-injection	0.001310 (0.0005902)
Brain@3-4 hours post-injection	0.001279 (0.0007786)
Heart Wall@20-30 minutes post-injection	0.009010 (0.0014472)
Heart Wall@1 hour post-injection	0.006371 (0.0012260)
Heart Wall@2 hours post-injection	0.004330 (0.0014781)
Heart Wall@3-4 hours post-injection	0.003209 (0.0014961)
Kidney@20-30 minutes post-injection	0.033219 (0.0140235)
Kidney@1 hour post-injection	0.022069 (0.0090106)
Kidney@2 hours post-injection	0.018424 (0.0068331)
Kidney@3-4 hours post-injection	0.015772 (0.0069341)
Lacrimal Gland@20-30 minutes post-injection	0.000016 (0.0000023)
Lacrimal Gland@1 hour post-injection	0.000016 (0.0000051)
Lacrimal Gland@2 hours post-injection	0.000015 (0.0000045)
Lacrimal Gland@3-4 hours post-injection	0.000014 (0.0000074)
Liver@20-30 minutes post-injection	0.040546 (0.0098781)
Liver@1 hour post-injection	0.030958 (0.0073605)
Liver@2 hours post-injection	0.023145 (0.0083627)
Liver@3-4 hours post-injection	0.018128 (0.0081345)
Lungs@20-30 minutes post-injection	0.010066 (0.0017280)
Lungs@1 hour post-injection	0.007535 (0.0013048)
Lungs@2 hours post-injection	0.005023 (0.0015987)
Lungs@3-4 hours post-injection	0.003601 (0.0016623)
Salivary Gland@20-30 minutes post-injection	0.002001 (0.0004118)
Salivary Gland@1 hour post-injection	0.001585 (0.0004877)
Salivary Gland@2 hours post-injection	0.001282 (0.0006661)
Salivary Gland@3-4 hours post-injection	0.001032 (0.0005455)
Spleen@20-30 minutes post-injection	0.003712 (0.0010597)
Spleen@1 hour post-injection	0.002645 (0.0008966)
Spleen@2 hours post-injection	0.001724 (0.0007601)
Spleen@3-4 hours post-injection	0.001264 (0.0006056)
Thyroid@20-30 minutes post-injection	0.000378 (NA)
Thyroid@1 hour post-injection	0.000266 (NA)
Thyroid@2 hours post-injection	0.000201 (NA)
Thyroid@3-4 hours post-injection	0.000128 (NA)

3. Secondary Outcome

Title	Phase I: Urinary Excretion of [68Ga]-PSMA-R2
Description	Urine samples were collected (up to 6 hours after dosing) for activity-based pharmacokinetics characterization. The apparent systemic clearance for the analyte in urine (Cl) was summarized with descriptive statistics.
Time Frame	0 to 6 hours post-dose

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS).

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Mean (Standard Deviation) [mL/hr]	5870 (1820)

4. Secondary Outcome

Title	Phase I: Half-life of 68Ga-PSMA-R2 in Blood
Description	Serial blood samples were collected (up to 6 hours after dosing) for activity-based pharmacokinetics characterization. The half-life (T^1/2) for the analyte in blood was summarized with descriptive statistics.
Time Frame	0 to 6 hours post-dose

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS).

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Mean (Standard Deviation) [Hour]	2.83 (0.868)

5. Secondary Outcome

Title	Phase I: Non-decay Corrected Tissue Time-activity Curves (TACs) From 68Ga-PSMA-R2 PET/CT Images in Normal Organs
Description	PET/CT scans were performed at approximately 20 to 30 min and at 1, 2, 3 to 4 hours postinjection. Time activity curves (TACs) for the various organs were produced as non-decay-corrected fraction of injected activity (mSv/MBq) per organ. Only descriptive analysis performed.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (20-30 min post-injection, 1 hour, 2 hours and 3-4 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS). Only participants with a value at each post-injection timepoints were included in the analysis.

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Brain@20-30 minutes post-injection	0.001686 (0.0007242)
Brain@1 hour post-injection	0.001046 (0.0000814)
Brain@2 hours post-injection	0.000423 (0.0001630)
Brain@3-4 hours post-injection	0.000222 (0.0000924)
Heart Wall@20-30 minutes post-injection	0.006914 (0.0011156)
Heart Wall@1 hour post-injection	0.003484 (0.0004766)
Heart Wall@2 hours post-injection	0.001332 (0.0002056)
Heart Wall@3-4 hours post-injection	0.000542 (0.0001255)
Kidney@20-30 minutes post-injection	0.025506 (0.0107777)
Kidney@1 hour post-injection	0.012059 (0.0043426)
Kidney@2 hours post-injection	0.005825 (0.0015596)
Kidney@3-4 hours post-injection	0.002766 (0.0006581)
Lacrimal Gland@20-30 minutes post-injection	0.000012 (0.0000019)
Lacrimal Gland@1 hour post-injection	0.000009 (0.0000022)
Lacrimal Gland@2 hours post-injection	0.000005 (0.0000011)
Lacrimal Gland@3-4 hours post-injection	0.000002 (0.0000008)
Liver@20-30 minutes post-injection	0.031128 (0.0076342)
Liver@1 hour post-injection	0.016949 (0.0032692)
Liver@2 hours post-injection	0.007172 (0.0014994)
Liver@3-4 hours post-injection	0.003087 (0.0006828)
Lungs@20-30 minutes post-injection	0.007729 (0.0013599)
Lungs@1 hour post-injection	0.004149 (0.0006660)
Lungs@2 hours post-injection	0.001573 (0.0002652)
Lungs@3-4 hours post-injection	0.000631 (0.0001601)
Salivary Gland@20-30 minutes post-injection	0.001536 (0.0003192)
Salivary Gland@1 hour post-injection	0.000859 (0.0002093)
Salivary Gland@2 hours post-injection	0.000386 (0.0001469)
Salivary Gland@3-4 hours post-injection	0.000173 (0.0000550)
Spleen@20-30 minutes post-injection	0.002849 (0.0008140)
Spleen@1 hour post-injection	0.001444 (0.0004213)
Spleen@2 hours post-injection	0.000536 (0.0001640)
Spleen@3-4 hours post-injection	0.000217 (0.0000567)
Thyroid@20-30 minutes post-injection	0.000289 (NA)
Thyroid@1 hour post-injection	0.000136 (NA)
Thyroid@2 hours post-injection	0.000057 (NA)
Thyroid@3-4 hours post-injection	0.000020 (NA)

6. Secondary Outcome

Title	Phase I: Residence Times in Normal Organs
Description	Residence times of radiation in normal organs were summarized with descriptive statistics.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS). For each parameter, only participants with a value are included in the analysis.

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Brain	0.002895 (0.0009849)
Heart	0.010459 (0.0014152)
Kidney	0.039360 (0.0133500)
Lacrimal Gland	0.000027 (0.0000052)
Liver	0.050735 (0.0103951)
Lungs	0.012084 (0.0019321)
Salivary Gland	0.002594 (0.0006622)
Spleen	0.004291 (0.0012416)
Thyroid	0.000424 (NA)
Urinary Bladder	0.092947 (0.0453608)
Remainder	1.417135 (0.0582923)

7. Secondary Outcome

Title	Phase I: Absorbed Dose of 68Ga-PSMA-R2
Description	Absorbed radiation dose of 68Ga-PSMA-R2 in target organs were summarized with descriptive statistics.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS).

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Brain	0.002563 (0.000336)
Heart	0.018417 (0.0020094)
Kidney	0.060683 (0.0190588)
Lacrimal Gland	0.008065 (0.0015741)
Liver	0.017417 (0.0029976)
Lungs	0.007967 (0.0007718)
Red Marrow	0.010700 (0.0002280)
Salivary Gland	0.015600 (0.0032012)
Spleen	0.017333 (0.0037109)
Urinary Bladder	0.120317 (0.0517023)

8. Secondary Outcome

Title	Phase I: Whole-body Dose of 68Ga-PSMA-R2
Description	The whole-body dose of 68Ga-PSMA-R2 was summarized with descriptive statistics.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Mean (Standard Deviation) [mGy/MBq]	0.013800 (0.0000632)

9. Secondary Outcome

Title	Phase I: Effective Dose of 68Ga-PSMA-R2
Description	The effective dose of 68Ga-PSMA-R2 was summarized with descriptive statistics.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6
Mean (Standard Deviation) [mSv/MBq]	0.014583 (0.0019343)

10. Secondary Outcome

Title	Standard Uptake Value (SUV) Mean and Max in Lesions Detected by PET Scans by Timepoint
Description	Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The SUVmean and SUVmax (g/mL) of each lesion were calculated and reported by lesion location with summary statistics at all imaging time points.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET (1hr): SUVmax (lesion)	4.493 (1.4060)	4.421 (1.4512)	6.725 (5.5327)
PET (1hr): SUVmean (background)	0.980 (0.0283)	0.643 (0.2318)	0.750 (0.3002)
PET (2hr): SUVmax (lesion)	3.767 (1.1493)	5.098 (1.8597)	6.846 (4.7745)
PET (2hr): SUVmean (background)	0.630 (0.3145)	0.651 (0.2817)	0.550 (0.1948)

11. Secondary Outcome

Title	Tumor to Background Ratio (TBR) of Lesions Detected by PET Scans by Timepoint
Description	Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The lesion Tumor to Background Ratio (TBR) was defined as SUVmax(lesion) / SUVmean(gluteal or thigh) was calculated and reported by lesion location with summary statistics at all imaging time points.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET (1hr): TBR	4.520 (1.3558)	7.464 (3.0364)	11.141 (10.6283)
PET (2hr): TBR	5.694 (1.7104)	7.780 (3.6034)	12.588 (9.1146)

12. Secondary Outcome

Title	Standard Uptake Value (SUV) Mean and Max in Lesions Detected by PET Scans and Also Detected by Conventional Scans by Timepoint
Description	Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The SUVmean and SUVmax (g/mL) of each lesion were calculated and reported by lesion location with summary statistics at all imaging time points.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS). Only participants with at least 1 positive lesion detected by conventional scan and at least 1 positive lesion detected by PET included in the analysis.

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET (1hr): SUVmax (lesion)	7.087 (4.9133)
PET (1hr): SUVmean (background)	0.689 (0.1955)
PET (2hr): SUVmax (lesion)	7.647 (5.3409)
PET (2hr): SUVmean (background)	0.541 (0.2234)

13. Secondary Outcome

Title	Tumor to Background Ratio (TBR) of Lesions Detected by PET Scans and Also Detected by Conventional Scans by Timepoint
Description	Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The lesion Tumor to Background Ratio (TBR) was defined as SUVmax(lesion) / SUVmean(gluteal or thigh) was calculated and reported by lesion location with summary statistics at all imaging time points.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS). Only participants with at least 1 positive lesion detected by conventional scan and at least 1 positive lesion detected by PET included in the analysis.

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET (1hr): TBR	11.573 (10.2632)
PET (2hr): TBR	14.880 (10.1991)

14. Secondary Outcome

Title	Standard Uptake Value (SUV) Mean and Max in Lesions Detected by PET Scans and Not Detected by Conventional Scans by Timepoint
Description	Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The SUVmean and SUVmax (g/mL) of each lesion were calculated and reported by lesion location with summary statistics at all imaging time points.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET (1hr): SUVmax (lesion)	4.493 (1.4060)	4.421 (1.4512)	6.578 (5.8224)
PET (1hr): SUVmean (background)	0.980 (0.0283)	0.643 (0.2318)	0.723 (0.3020)
PET (2hr): SUVmax (lesion)	3.767 (1.1493)	5.098 (1.8597)	6.566 (4.5956)
PET (2hr): SUVmean (background)	0.630 (0.3145)	0.651 (0.2817)	0.581 (0.2119)

15. Secondary Outcome

Title	Tumor to Background Ratio (TBR) of Lesions Detected by PET Scans and Not Detected by Conventional Scans by Timepoint
Description	Targeting properties of 68Ga-PSMA-R2 were evaluated by semi-quantitatively assessing radiotracer uptake at lesion level, identified via PET/CT imaging (4 scans). The lesion Tumor to Background Ratio (TBR) was defined as SUVmax(lesion) / SUVmean(gluteal or thigh) was calculated and reported by lesion location with summary statistics at all imaging time points.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET (1hr): TBR	4.520 (1.3558)	7.464 (3.0364)	10.965 (10.9067)
PET (2hr): TBR	5.694 (1.7104)	7.780 (3.6034)	11.788 (8.6914)

16. Secondary Outcome

Title	Patient Level Agreement of 68Ga-PSMA-R2 PET Imaging Relative to Conventional Techniques in Prostate Cancer Patients
Description	The subject-level positive percent agreement, negative percent agreement, and overall percent agreement was calculated based on the number of subjects with at least 1 positive lesion detected by conventional scan or at least 1 positive lesion detected by PET scan. These percent agreements were calculated as follows: Positive percent agreement: a/(a+c) × 100 Negative percent agreement: d/(b+d) × 100 Overall percent agreement: (a+d)/(a+b+c+d) × 100 Where: a = number of subjects with at least 1 positive lesion detected by conventional scan and at least 1 positive lesion detected by PET scan b = number of subjects with at least 1 positive lesion detected by PET scan that was not correlated with conventional scan c = number of subjects with at least 1 positive lesion detected by conventional scan that was not correlated with PET scan d = number of subjects with no lesions detected by conventional scan or PET scan.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour, 2 hours post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)	Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	6	12	12
PET(1hr): Positive percent agreement	0.0	0.0	87.5
PET(1hr): Negative percent agreement	66.7	25.0	0.0
PET(1hr): Overall percent agreement	66.7	25.0	58.3
PET(2hr): Positive percent agreement	0.0	0.0	87.5
PET(2hr): Negative percent agreement	33.3	25.0	50.0
PET(2hr): Overall percent agreement	33.3	5.49	75.0

17. Secondary Outcome

Title	Burden of Tumor Lesions Measured by 68Ga-PSMA-R2 PET (1hr) Scan Compared With Standard Imaging Modality, by Location (Overall)
Description	The differences of number of positive lesions, number of positive lesions detected by PET scan and/or conventional scan and the location of positive lesions were summarized with descriptive statistics.
Time Frame	68Ga-PSMA-R2 PET imaging acquired at Day 1 (1 hour post-injection)

Outcome Measure Data

Analysis Population Description

Full Analysis Set (FAS)

Arm/Group Title	Overall
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
Measure Participants	30
PET (positive)	22
Conventional (postive)	8
Difference = PET(+) - Conventional(+)	14
PET(+) and detected by conventional scan	7
PET+/detected by CT:Bone,Cervical Spine	1
PET+/detected by CT:Bone,Lumbar Spine	3
PET+/detected by CT:Bone,Thoracic Spine	3
PET+/detected by CT:Pelvic Bone	2
PET+/detected by CT:Pelvis	1
PET+/detected by CT:Rib(s),L.	1
PET+/detected by CT:Rib(s),R.	1
PET(+) and not detected by conventional scan	21
PET+/undetected by CT:Abdominal Wall	1
PET+/undetected by CT:Bone,Lumbar Spine	1
PET+/undetected by CT:Bone,Other	5
PET+/undetected by CT:Bone,Thoracic Spine	1
PET+/undetected by CT:Lymph Node,Common Iliac	9
PET+/undetected by CT:Lymph Node,External	1
PET+/undetected by CT:Lymph Node,Inguinal,L.	1
PET+/undetected by CT:Lymph Node,Inguinal,R.	1
PET+/undetected by CT:Lymph Node,Para-Aortic	6
PET+/undetected by CT:Lymph Node,Retrocrural	1
PET+/undetected by CT:Lymph Node,Retroperitoneal	2
PET+/undetected by CT:Lymph Node,Supraclavicular,L	1
PET+/undetected by CT:Other,Extranodal	3
PET+/undetected by CT:Other,Nodal	3
PET+/undetected by CT:Pelvic Bone	6
PET+/undetected by CT:Rib(s),L.	1
PET+/undetected by CT:Rib(s),R.	2
PET+/undetected by CT:Urethra	1
Conventional (+) and not detected by PET scan	7
CT+/undetected by PET:Bone,Lumbar Spine	2
CT+/undetected by PET:Bone,Other	2
CT+/undetected by PET:Bone,Thoracic Spine	5
CT+/undetected by PET:Lymph Node,Pelvic	1
CT+/undetected by PET:Pelvic Bone	6
CT+/undetected by PET:Rib(s),L.	2
CT+/undetected by PET:Rib(s),R.	1
CT+/undetected by PET:Skull	1

Adverse Events

Time Frame	Adverse events (AEs) were collected from informed consent signature through study completion, an average of 4 weeks.
Adverse Event Reporting Description	Any sign or symptom that occurs after written informed consent provided. For TEAE from first dosing (single administration, Day 1) up to last follow-up visit or until the event has resolved to baseline grade or better or the event was assessed stable by the investigator or the patient was lost to follow-up or withdrew consent.
Arm/Group Title	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)		Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)		Metastatic Prostate Cancer (mPCa) (Phase II)
Arm/Group Description	All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].		All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].		All eligible participants received recommended dose of [68Ga]-PSMA-R2 of 3 Mega Becquerel (MBq)/Kg (+/- 10%) [but not more than 250 and not less than 150 MBq].
All Cause Mortality
	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)		Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)		Metastatic Prostate Cancer (mPCa) (Phase II)
	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events
Total	0/6 (0%)		0/12 (0%)		0/12 (0%)
Serious Adverse Events
	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)		Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)		Metastatic Prostate Cancer (mPCa) (Phase II)
	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events
Total	0/6 (0%)		1/12 (8.3%)		0/12 (0%)
Gastrointestinal disorders
Ileus	0/6 (0%)		1/12 (8.3%)		0/12 (0%)
Other (Not Including Serious) Adverse Events
	Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase I)		Biochemically Recurrent Prostate Cancer (PCa-BR) (Phase II)		Metastatic Prostate Cancer (mPCa) (Phase II)
	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events	Affected / at Risk (%)	# Events
Total	1/6 (16.7%)		4/12 (33.3%)		2/12 (16.7%)
Blood and lymphatic system disorders
Leukocytosis	1/6 (16.7%)		0/12 (0%)		0/12 (0%)
General disorders
Fatigue	0/6 (0%)		2/12 (16.7%)		1/12 (8.3%)
Influenza like illness	0/6 (0%)		1/12 (8.3%)		0/12 (0%)
Pyrexia	0/6 (0%)		1/12 (8.3%)		0/12 (0%)
Nervous system disorders
Dysgeusia	0/6 (0%)		1/12 (8.3%)		0/12 (0%)
Headache	0/6 (0%)		0/12 (0%)		1/12 (8.3%)
Renal and urinary disorders
Dysuria	0/6 (0%)		0/12 (0%)		1/12 (8.3%)
Respiratory, thoracic and mediastinal disorders
Cough	0/6 (0%)		0/12 (0%)		1/12 (8.3%)
Skin and subcutaneous tissue disorders
Rash	0/6 (0%)		1/12 (8.3%)		1/12 (8.3%)

Limitations/Caveats

[Not Specified]

More Information

Certain Agreements

Principal Investigators are NOT employed by the organization sponsoring the study.

The terms and conditions of Novartis' agreements with its investigators may vary. However, Novartis does not prohibit any investigator from publishing. Any publications from a single-site are postponed until the publication of the pooled data (ie, data from all sites) in the clinical trial.